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ChEMBL ligand: CHEMBL41036 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] | ||||||||
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay | B | 8.11 | pKi | 7.79 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
ChEMBL | Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay | B | 8.14 | pKi | 7.18 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314] |
ChEMBL | Binding affinity to TRalpha1 | B | 8.14 | pKi | 7.18 | nM | Ki | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Inhibition of thyroid hormone receptor alpha | B | 7.6 | pIC50 | 25.12 | nM | IC50 | Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994] |
GtoPdb | - | - | 7.6 | pIC50 | - | - | - | J Med Chem (2003) 46: 1580-8 [PMID:12699376] |
ChEMBL | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor alpha) was determined | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Inhibitory concentration against cloned human thyroid hormone receptor alpha 1 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653] |
ChEMBL | Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524] |
ChEMBL | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined | B | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
ChEMBL | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912] |
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
ChEMBL | Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay | B | 9.43 | pKi | 0.37 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314] |
ChEMBL | Binding affinity to TRbeta1 | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
ChEMBL | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Inhibitory concentration against cloned human thyroid hormone receptor beta 1 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653] |
ChEMBL | Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524] |
GtoPdb | - | - | 8.96 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2003) 100: 10067-72 [PMID:12888625] |
ChEMBL | Inhibition of human thyroid hormone receptor beta 1 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2007) 15: 5251-5261 [PMID:17524652] |
ChEMBL | Inhibition of thyroid hormone receptor beta | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994] |
ChEMBL | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | B | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
ChEMBL | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined | B | 8.46 | pEC50 | 3.5 | nM | EC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay | F | 8.95 | pEC50 | 1.12 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]